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Assay Detail

CHEMBL3266609

Review assay metadata, readout intent, target linkage, and publication context from the same page.

ADMET
Inhibition of CYP2C9 (unknown origin)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia.
Kelly MJ, Pietranico-Cole S, Larigan JD, Haynes NE, Reynolds CH, Scott N, Vermeulen J, Dvorozniak M, Conde-Knape K, Huang KS, So SS, Thakkar K, Qian Y, Banner B, Mennona F, Danzi S, Klein I, Taub R, Tilley J.
J Med Chem (2014) 57 : 3912 -3923
PubMed 24712661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.66 4.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3261331 RESMETIROM 4.0 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3261331 RESMETIROM IC50 = 22000.0 nM 4.66